2. Signaling Pathways
  3. Membrane Transporter/Ion Channel
    Neuronal Signaling
  4. GABA Receptor

GABA Receptor

Gamma-aminobutyric acid Receptor; γ-Aminobutyric acid Receptor

GABA Receptor

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GABA receptors are a class of receptors that respond to the neurotransmitter gamma-aminobutyric acid (GABA), the chief inhibitory neurotransmitter in the vertebrate central nervous system. There are two classes of GABA receptors: GABAA and GABAB. GABAA receptors are ligand-gated ion channels (also known as ionotropic receptors), whereas GABAB receptors are G protein-coupled receptors (also known asmetabotropic receptors). It has long been recognized that the fast response of neurons to GABA that is blocked by bicuculline and picrotoxin is due to direct activation of an anion channel. This channel was subsequently termed the GABAA receptor. Fast-responding GABA receptors are members of family of Cys-loop ligand-gated ion channels. A slow response to GABA is mediated by GABAB receptors, originally defined on the basis of pharmacological properties.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-111052R
    AZD7325 (Standard)
    		Agonist
    AZD7325 (Standard) is the analytical standard of AZD7325. This product is intended for research and analytical applications. AZD7325 is a potent and orally active partial selective PAM of GABAAα2 and Aα3 receptor (Ki=0.3 and 1.3 nM, respectively), and has less antagonistic efficacy at the Aα1 and Aα5 receptor subtypes. AZD7325 is a moderate CYP1A2 and a potent CYP3A4 inducer in vitro. AZD7325 has the potential for the investigation of anxiety and dravet syndrome. PAM: positive allosteric modulator.
    AZD7325 (Standard)
  • HY-B1326R
    Bemegride (Standard)
    		Antagonist
    Bemegride (Standard) is the analytical standard of Bemegride. This product is intended for research and analytical applications. Bemegride (3-Ethyl-3-methylglutarimide) is a central nervous system stimulant and antidote for barbiturate poisoning.
    Bemegride (Standard)
  • HY-N1951R
    Miltirone (Standard)
    		Agonist
    Miltirone is an orally active natural compound found in the root of Salvia miltiorrhiza. Miltirone is a central benzodiazepine receptor partial agonist, with an IC50 of 0.3 μM. Miltirone induces ROS - and-p53 dependent apoptosis. Miltirone inhibits carboxylesterase 2 (CES2; Ki = 0.04 μM) and SARS-CoV main protease (Mpro).
    Miltirone (Standard)
  • HY-107489R
    RO 4938581 (Standard)
    		Antagonist
    RO 4938581 (Standard) is the analytical standard of RO 4938581 (HY-107489). This product is intended for research and analytical applications. RO 4938581 is a potent and selective GABAA α5 inverse agonist, with a Ki of 4.6 nM for GABAA α5β3γ2a, and shows a lower affinity at α1β3γ2a, α2β3γ2a, α3β3γ2a (Ki, 174, 185, 80 nM, respectively); RO 4938581 is used in the research of cognitive dysfunction.
    RO 4938581 (Standard)
  • HY-120192
    CGP 62349
    		Antagonist
    CGP 62349 is a selective and orally active GABAB receptor antagonist that improves cognitive performance in multiple learning paradigms.
    CGP 62349
  • HY-10232R
    THIP (Standard)
    		Antagonist
    THIP (Standard) is the analytical standard of THIP. This product is intended for research and analytical applications. THIP (Gaboxadol) is a selective extrasynaptic GABAA receptors (eGABARs) agonist (with blood-brain barrier permeability), shows an EC50 value of 13 μM for δ-GABAAR. THIP induces strong tense GABAA-mediated currents in layer 2/3 neurons, but shows on effect on miniature IPSCs. THIP can be used in studies of sleep disorders.
    THIP (Standard)
  • HY-N2368AR
    Arecaidine hydrochloride (Standard)
    		Inhibitor
    Arecaidine hydrochloride, a pyridine alkaloid, is a potent GABA uptake inhibitor. Arecaidine hydrochloride is a substrate of H+-coupled amino acid transporter 1 (PAT1, SLC36A1) and competitively inhibits L-proline uptake.
    Arecaidine hydrochloride (Standard)
  • HY-121599R
    CGP 36742 (Standard)
    		Antagonist
    CGP 36742 (Standard) is the analytical standard of CGP 36742. This product is intended for research and analytical applications. CGP 36742 (SGS-742) is an orally active and selective antagonist of GABAB receptor (IC50 = 36 µM). CGP 36742 is a brain-penetrant compound and improves cognitive performances. CGP 36742 can be used for depression study.
    CGP 36742 (Standard)
  • HY-B0122SS1
    Topiramate-13C6-1
    		Activator
    Topiramate-13C6-1 (McN 4853-13C6-1; RWJ 17021-13C6-1) is 13C-labeled Topiramate (HY-B0122).
    Topiramate-<sup>13</sup>C<sub>6</sub>-1
  • HY-168363
    Ciclotizolam
    		Ligand
    Ciclotizolam (WE-973) is a thienotriazolodiazepine with anticonvulsant and anti-aggressive activities. Ciclotizolam binds to benzodiazepine receptors in the central nervous system. Ciclotizolam decreases total sleep time in cats.
    Ciclotizolam
  • HY-16579AS2
    Etifoxine-d5
    		Activator
    Etifoxine-d5 is the deuterium labeled Etifoxine. Etifoxine, a non-benzodiazepine GABAergic compound, is a positive allosteric modulator of α1β2γ2 and α1β3γ2 subunit-containing GABAA receptors. Etifoxine reveals anxiolytic and anticonvulsant properties in rodents.
    Etifoxine-d<sub>5</sub>
  • HY-103476R
    Ro15-4513 (Standard)
    		Antagonist
    Ro15-4513 (Standard) is the analytical standard of Ro15-4513. This product is intended for research and analytical applications. Ro15-4513, imidazobenzodiazepinone derivative, is a partial inverse agonist of benzodiazepine receptor (BZR). Ro15-4513 is a potent ethanol antagonist. Ro15-4513 has anti-anxiety effect. Ro15-4513 is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.
    Ro15-4513 (Standard)
  • HY-129090
    CGS-​9895
    		Antagonist
    CGS-​9895 is a GABA antagonist that acts via the benzodiazepine binding site of ag containing GABA receptors.
    CGS-​9895
  • HY-129105R
    Clomethiazole (Standard)
    		Agonist
    Clomethiazole (Standard) is the analytical standard of Clomethiazole. This product is intended for research and analytical applications. Chlormethiazole is an potent and orally active GABAA agonist. Chlormethiazole inhibits cytochrome P450 isoforms: CYP2A6 and CYP2E1 in human liver microsomes. Chlormethiazole is an anticonvulsant agent and has the potential for treating convulsive status epilepticus.
    Clomethiazole (Standard)
  • HY-17001R
    Flupirtine Maleate (Standard)
    		Activator
    Flupirtine Maleate (Standard) is the analytical standard of Flupirtine Maleate (HY-17001). This product is intended for research and analytical applications. Flupirtine Maleate is an orally active, blood-brain barrier-crossing non-opioid analgesic and neuroprotective agent. Flupirtine Maleate is a neuronal potassium channel opener (Kv7 activator), a NMDA receptor antagonist and a GABA receptor activator. Flupirtine Maleate stabilizes blood-brain-barrier integrity, reduces oxidative stress and brain leukocyte infiltration, enhances angioneurogenesis, suppresses calcium influx, stabilizes neuronal resting membrane potential, and counteracts focal cerebral ischemia. Flupirtine Maleate exhibits analgesic, muscle relaxant properties, protects neurons from excitotoxic, ischemic, or cytokine-mediated death. Flupirtine Maleate functions as a non-opioid analgesic without antipyretic or antiphlogistic properties, shows no relevant affinity to opiate receptor. Flupirtine Maleate can be used for the research of focal cerebral ischemia, pain, Alzheimer’s disease, or multiple sclerosis.
    Flupirtine Maleate (Standard)
  • HY-123426
    JY-XHe-053
    		Agonist
    JY-XHe-053 is a potent and selective agonist of GABAA receptors containing the α5 subunit (Kis of 22.0 nM, 12.3 nM, 34.9 nM, 0.7 nM for α1, α2, α3, α5, respectively). JY-XHe-053 lacks significant anti-anxiety activity, despite its efficacy at α2- and α3-GABAA receptors.
    JY-XHe-053
  • HY-19082
    Y-23684
    		Agonist
    Y-23684 is a partial agonist of benzodiazepine receptor (BZR) with anticonvulsant and anxiolytic activities. Y-23684 can be used in the research of treatment of anxiety disorders.
    Y-23684
  • HY-W013150R
    Alpidem (Standard)
    		Modulator
    Alpidem (Standard) is the analytical standard of Alpidem (HY-W013150). This product is intended for research and analytical applications. Alpidem, an anxiolytic agent, is an orally active and brain-penetrant GABAA receptor ligand, binds to α1β2γ2 subunit-containing GABAA receptors (IC50 of 17 nM) over α5β2γ2 subunit-containing GABAA receptors (IC50 of >10 μM). Alpidem modulates calcium-induced mitochondrial permeability transition, induces glutathione depletion and hepatocyte necrosis, potentiates TNF-α toxicity, inhibits marble-burying and locomotor activity, enhances stressed rodent feeding behavior, and exerts anticonvulsant effects. Alpidem can be used for the research of anxiety, anxiety disorders, and convulsions.
    Alpidem (Standard)
  • HY-101808R
    Doxefazepam (Standard)
    Doxefazepam (Standard) (SAS-643 (Standard)) is the analytical standard of Doxefazepam (HY-101808). This product is intended for research and analytical applications. Doxefazepam is a benzodiazepine derivative. It possesses anxiolytic, anticonvulsan and skeletal muscle relaxant properties.
    Doxefazepam (Standard)
  • HY-117257
    PF-0713
    		Agonist
    PF 0713 is a GABAA receptor agonist..
    PF-0713
Cat. No. Product Name / Synonyms Application Reactivity